Design, synthesis, and pharmacological evaluation of new farnesyl protein transferase inhibitors

…, JF Goossens, P Chavatte, JP Hénichart

Index: Houssin, Raymond; Pommery, Jean; Salauen, Marie-Catherine; Deweer, Sophie; Goossens, Jean-Francois; Chavatte, Philippe; Henichart, Jean-Pierre Journal of Medicinal Chemistry, 2002 , vol. 45, # 2 p. 533 - 536

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Citation Number: 27

Abstract

New CA1A2X peptidomimetics are described as Ras farnesyl transferase inhibitors (FTIs). They include cysteine and methionine as mimetics of the C-terminus sequence of farnesylated proteins. Furthermore, cysteine was replaced by heterocycles, taking into account the role of zinc and the metabolic instability of amino acids. The molecular docking of 8 in the active site of the enzyme and the pharmacological evaluation of the compounds ...